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Assay Detail

CHEMBL4771179

Review assay metadata, readout intent, target linkage, and publication context from the same page.

ADMET
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.
Nizi MG,Desantis J,Nakatani Y,Massari S,Mazzarella MA,Shetye G,Sabatini S,Barreca ML,Manfroni G,Felicetti T,Rushton-Green R,Hards K,Latacz G,Satała G,Bojarski AJ,Cecchetti V,Kolář MH,Handzlik J,Cook GM,Franzblau SG,Tabarrini O
Eur J Med Chem (2020) 201 : 112420 -112420
PubMed 32526553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.01 6.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479 THIORIDAZINE 4.0 1 6.74
CHEMBL4797066 1 6.00
CHEMBL4791959 1 5.67
CHEMBL4778666 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479 THIORIDAZINE Ki = 181.0 nM 6.74
CHEMBL4797066 Ki = 1003.0 nM 6.00
CHEMBL4791959 Ki = 2149.0 nM 5.67
CHEMBL4778666 Ki = 2340.0 nM 5.63